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Dihydroquinoxalinones and dihydropyrididopyrazinones modified BET protein inhibitors
专利权人:
Bayer Pharma Aktiengesellschaft
发明人:
SCHMEES, Norbert,HAENDLER, Bernard,STÖCKIGT, Detlef,GALLENKAMP, Daniel,BISSELL, Richard,BOUGLAS, Richard
申请号:
ES14737225
公开号:
ES2635003T3
申请日:
2014.07.07
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Compounds of general formula (I) ** Formula ** in which A represents -NH-, -N (C1-C3 alkyl) - or -O-, X represents -N- or -CH-, n represents 0, 1 or 2, R1 represents a group -C (>; = O) NR7R8 or -S (>; = O) 2NR7R8, or represents 5-membered monocyclic heteroaryl, which may eventually be mono-, di- or trisubstituted, in the same or different manner with halogen, cyano, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, halo-C1-C4 alkyl, C1-C4 alkoxy, halo-C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 halo-alkylthio , -NR9R10, -C (>; = O) OR11, -C (>; = O) N9R10, -C (>; = O) R11, -S (>; = O) 2R11, -S (>; = O) 2NR9R10, R2 represents hydrogen, halogen, cyano, C1-C3 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, halo-C1-C4 alkyl, C1-C4 alkoxy, halo-C1-C4 alkoxy, C1-C4 alkylthio or C1-halo alkyl -C4, and if n represents 2, R2 can be the same or different, or R1 and R2 together represent a group * -S (>; = O) 2-NR8-CH2 - **, * -S (>; = O) 2-NR8-CH2-CH2 - **, * -C (>; = O) -NR8-CH2 - ** or * - C (>; = O) -NR8-CH2-CH2 - **, where "*" means point d The bond of R1 to the phenyl ring contained in formula (I), and wherein "**" means a carbon atom of this phenyl ring adjacent to this bond point, R3 represents methyl or ethyl, R4 represents hydrogen or C1-C3 alkyl, R5 represents hydrogen or C1-C3 alkyl, or R4 and R5 together with the carbon atom to which they are attached represent C3-C6 cycloalkylene, R6 represents C1-C6 alkyl, which may eventually be monosubstituted with C1- alkoxy C3, phenyl, C3-C8 cycloalkyl or 4- to 8-membered heterocycloalkyl, where phenyl, in turn, may be mono-, di- or trisubstituted, in the same or different manner with: halogen, cyano, C1-C4 alkyl, alkenyl C2-C4, C2-C4 alkynyl, C1-C4 alkoxy, halo-C1-C4 alkyl, halo-C1-C4 alkoxy, and wherein C3-C8 cycloalkyl and 4- to 8-membered heterocycloalkyl may eventually be mono- or disubstituted, in the same or different manner with C1-C3 alkyl, or represents C3-C8 cycloalkyl or heterocycle alkyl of 4 to 8 members, which m
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